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Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior. / Butini, Stefania; Gemma, Sandra; Campiani, Giuseppe; Franceschini, Silvia; Trotta, Francesco; Borriello, Marianna; Ceres, Nicoletta; Ros, Sindu; Coccone, Salvatore Sanna; Bernetti, Matteo; De Angelis, Meri; Brindisi, Margherita; Nacci, Vito; Fiorini, Isabella; Novellino, Ettore; Cagnotto, Alfredo; Mennini, Tiziana; Sandager-Nielsen, Karin; Andreasen, Jesper Tobias; Scheel-Kruger, Jorgen; Mikkelsen, Jens D; Fattorusso, Caterina.
In:
Journal of Medicinal Chemistry, Vol. 52, No. 1, 2009, p. 151-69.
Research output: Contribution to journal › Journal article › Research › peer-review
Harvard
Butini, S, Gemma, S, Campiani, G, Franceschini, S, Trotta, F, Borriello, M, Ceres, N, Ros, S, Coccone, SS, Bernetti, M, De Angelis, M, Brindisi, M, Nacci, V, Fiorini, I, Novellino, E, Cagnotto, A, Mennini, T, Sandager-Nielsen, K, Andreasen, JT, Scheel-Kruger, J
, Mikkelsen, JD & Fattorusso, C 2009, '
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior',
Journal of Medicinal Chemistry, vol. 52, no. 1, pp. 151-69.
https://doi.org/10.1021/jm800689gAPA
Butini, S., Gemma, S., Campiani, G., Franceschini, S., Trotta, F., Borriello, M., Ceres, N., Ros, S., Coccone, S. S., Bernetti, M., De Angelis, M., Brindisi, M., Nacci, V., Fiorini, I., Novellino, E., Cagnotto, A., Mennini, T., Sandager-Nielsen, K., Andreasen, J. T., ... Fattorusso, C. (2009).
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
Journal of Medicinal Chemistry,
52(1), 151-69.
https://doi.org/10.1021/jm800689gVancouver
Butini S, Gemma S, Campiani G, Franceschini S, Trotta F, Borriello M et al.
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
Journal of Medicinal Chemistry. 2009;52(1):151-69.
https://doi.org/10.1021/jm800689gAuthor
Butini, Stefania ; Gemma, Sandra ; Campiani, Giuseppe ; Franceschini, Silvia ; Trotta, Francesco ; Borriello, Marianna ; Ceres, Nicoletta ; Ros, Sindu ; Coccone, Salvatore Sanna ; Bernetti, Matteo ; De Angelis, Meri ; Brindisi, Margherita ; Nacci, Vito ; Fiorini, Isabella ; Novellino, Ettore ; Cagnotto, Alfredo ; Mennini, Tiziana ; Sandager-Nielsen, Karin ; Andreasen, Jesper Tobias ; Scheel-Kruger, Jorgen ; Mikkelsen, Jens D ; Fattorusso, Caterina. / Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior. In: Journal of Medicinal Chemistry. 2009 ; Vol. 52, No. 1. pp. 151-69.
Bibtex
@article{3229ce1068a411df928f000ea68e967b,
title = "Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior",
abstract = "Dopamine D(3) antagonism combined with serotonin 5-HT(1A) and 5-HT(2A) receptor occupancy may represent a novel paradigm for developing innovative antipsychotics. The unique pharmacological features of 5i are a high affinity for dopamine D(3), serotonin 5-HT(1A) and 5-HT(2A) receptors, together with a low affinity for dopamine D(2) receptors (to minimize extrapyramidal side effects), serotonin 5-HT(2C) receptors (to reduce the risk of obesity under chronic treatment), and for hERG channels (to reduce incidence of torsade des pointes). Pharmacological and biochemical data, including specific c-fos expression in mesocorticolimbic areas, confirmed an atypical antipsychotic profile of 5i in vivo, characterized by the absence of catalepsy at antipsychotic dose.",
author = "Stefania Butini and Sandra Gemma and Giuseppe Campiani and Silvia Franceschini and Francesco Trotta and Marianna Borriello and Nicoletta Ceres and Sindu Ros and Coccone, {Salvatore Sanna} and Matteo Bernetti and {De Angelis}, Meri and Margherita Brindisi and Vito Nacci and Isabella Fiorini and Ettore Novellino and Alfredo Cagnotto and Tiziana Mennini and Karin Sandager-Nielsen and Andreasen, {Jesper Tobias} and Jorgen Scheel-Kruger and Mikkelsen, {Jens D} and Caterina Fattorusso",
note = "Keywords: Animals; Antipsychotic Agents; Behavior, Animal; Binding Sites; Drug Design; Drug Evaluation, Preclinical; Humans; Ligands; Mice; Models, Molecular; Molecular Structure; Protein Binding; Receptor, Serotonin, 5-HT1A; Receptor, Serotonin, 5-HT2A; Receptors, Dopamine D3; Structure-Activity Relationship",
year = "2009",
doi = "10.1021/jm800689g",
language = "English",
volume = "52",
pages = "151--69",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "1",
}
RIS
TY - JOUR
T1 - Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior
AU - Butini, Stefania
AU - Gemma, Sandra
AU - Campiani, Giuseppe
AU - Franceschini, Silvia
AU - Trotta, Francesco
AU - Borriello, Marianna
AU - Ceres, Nicoletta
AU - Ros, Sindu
AU - Coccone, Salvatore Sanna
AU - Bernetti, Matteo
AU - De Angelis, Meri
AU - Brindisi, Margherita
AU - Nacci, Vito
AU - Fiorini, Isabella
AU - Novellino, Ettore
AU - Cagnotto, Alfredo
AU - Mennini, Tiziana
AU - Sandager-Nielsen, Karin
AU - Andreasen, Jesper Tobias
AU - Scheel-Kruger, Jorgen
AU - Mikkelsen, Jens D
AU - Fattorusso, Caterina
N1 - Keywords: Animals; Antipsychotic Agents; Behavior, Animal; Binding Sites; Drug Design; Drug Evaluation, Preclinical; Humans; Ligands; Mice; Models, Molecular; Molecular Structure; Protein Binding; Receptor, Serotonin, 5-HT1A; Receptor, Serotonin, 5-HT2A; Receptors, Dopamine D3; Structure-Activity Relationship
PY - 2009
Y1 - 2009
N2 - Dopamine D(3) antagonism combined with serotonin 5-HT(1A) and 5-HT(2A) receptor occupancy may represent a novel paradigm for developing innovative antipsychotics. The unique pharmacological features of 5i are a high affinity for dopamine D(3), serotonin 5-HT(1A) and 5-HT(2A) receptors, together with a low affinity for dopamine D(2) receptors (to minimize extrapyramidal side effects), serotonin 5-HT(2C) receptors (to reduce the risk of obesity under chronic treatment), and for hERG channels (to reduce incidence of torsade des pointes). Pharmacological and biochemical data, including specific c-fos expression in mesocorticolimbic areas, confirmed an atypical antipsychotic profile of 5i in vivo, characterized by the absence of catalepsy at antipsychotic dose.
AB - Dopamine D(3) antagonism combined with serotonin 5-HT(1A) and 5-HT(2A) receptor occupancy may represent a novel paradigm for developing innovative antipsychotics. The unique pharmacological features of 5i are a high affinity for dopamine D(3), serotonin 5-HT(1A) and 5-HT(2A) receptors, together with a low affinity for dopamine D(2) receptors (to minimize extrapyramidal side effects), serotonin 5-HT(2C) receptors (to reduce the risk of obesity under chronic treatment), and for hERG channels (to reduce incidence of torsade des pointes). Pharmacological and biochemical data, including specific c-fos expression in mesocorticolimbic areas, confirmed an atypical antipsychotic profile of 5i in vivo, characterized by the absence of catalepsy at antipsychotic dose.
U2 - 10.1021/jm800689g
DO - 10.1021/jm800689g
M3 - Journal article
C2 - 19072656
VL - 52
SP - 151
EP - 169
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 1
ER -
